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    • 1. 发明授权
    • Method for producing powdery particle-reduced formulations with the aid of compressed gases
    • 借助于压缩气体生产粉末颗粒减少配方的方法
    • US06680284B1
    • 2004-01-20
    • US10030035
    • 2002-01-03
    • Jürgen HeidlasMartin OberJohann Wiesmüller
    • Jürgen HeidlasMartin OberJohann Wiesmüller
    • A01N2512
    • A61K9/14A61K9/1617Y10S514/959Y10S516/922Y10S516/928
    • For the preparation of pulverulent particle-reduced formulations with the aid of compressed gases, the solid compound to be formulated, a poorly soluble and usually bioactive active compound, is homogeneously ground together with 10-99% by weight (based on the formulation) of a carrier material which is essentially soluble in the compressed gas mixture, in the presence of compressed gas or mixtures thereof in a stirred autoclave having a mechanical grinding device at process temperatures between 10 and 200° C. and at process pressures between 5 and 500 bar, and in a second process stage the compressed gas mixture, usually dimethyl ether, pure propane and/or carbon dioxide, is expanded by lowering the pressure and separated off from the homogenate, which can also be present as a melt. Finally, the pulverulent particle-reduced formulation is recovered from the homogenate obtained, with which significant improvements in the solubility properties and in particular in the bioavailability of originally poorly soluble and nonsoluble compounds are to be achieved.
    • 为了在压缩气体的帮助下制备粉末颗粒减少的制剂,将待配制的固体化合物,难溶性和通常为生物活性的活性化合物与10-99重量%(基于制剂)均匀地研磨 在压缩气体或其混合物的存在下,基本上可溶于压缩气体混合物的载体材料在具有机械研磨装置的搅拌高压釜中,处理温度为10-200℃,过程压力为5至500巴 ,并且在第二工艺阶段,压缩气体混合物,通常是二甲醚,纯丙烷和/或二氧化碳,通过降低压力而膨胀,并从匀浆中分离,其也可以熔体形式存在。 最后,从获得的匀浆中回收粉末颗粒减少的制剂,其中可以实现溶解性能,特别是原始难溶性和不溶性化合物的生物利用度的显着改善。